Desgranges C, Razaka G, Rabaud M, Bricaud H, Balzarini J, De Clercq E
Biochem Pharmacol. 1983 Dec 1;32(23):3583-90. doi: 10.1016/0006-2952(83)90307-6.
Various 5-substituted-2'-deoxyuridines (dUrd), including 5-ethyl,5-propyl-, 5-trifluoromethyl-, 5-hydroxymethyl-, 5-formyl-, 5-vinyl-, (E)-5-(2-chlorovinyl)-, (E)-5-(2-bromovinyl)-, 5-fluoro-, 5-chloro-, 5-bromo-, 5-iodo-, 5-cyano-, 5-thiocyano-, 5-nitro- and 5-amino-dUrd, were shown to be effective substrates for the thymidine (dThd) phosphorylase isolated from human blood platelets. Some of dUrd analogs, i.e. the highly potent and selective antiherpes agent (E)-5-(2-bromovinyl)-dUrd, were degraded more rapidly than the natural substrates, dUrd and dThd. All dUrd analogs were also readily catabolised by intact human blood platelets. The potent inhibitors of thymidine phosphorylase, 6-amino-thymine and 6-amino-5-bromo-uracil, strongly inhibited the phosphorolysis of (E)-5-(2-bromovinyl)-dUrd by both purified enzyme and intact platelets.
各种5-取代-2'-脱氧尿苷（dUrd），包括5-乙基、5-丙基、5-三氟甲基、5-羟甲基、5-甲酰基、5-乙烯基、（E）-5-（2-氯乙烯基）、（E）-5-（2-溴乙烯基）、5-氟、5-氯、5-溴、5-碘、5-氰基、5-硫氰基、5-硝基和5-氨基-dUrd，已被证明是从人血小板中分离出的胸苷（dThd）磷酸化酶的有效底物。一些dUrd类似物，即高效且选择性的抗疱疹药物（E）-5-（2-溴乙烯基）-dUrd，比天然底物dUrd和dThd降解得更快。所有dUrd类似物也很容易被完整的人血小板分解代谢。胸苷磷酸化酶的强效抑制剂6-氨基胸腺嘧啶和6-氨基-5-溴尿嘧啶，强烈抑制纯化酶和完整血小板对（E）-5-（2-溴乙烯基）-dUrd的磷酸解作用。
